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US 6,310,262 B1Granted
Process for preparing retiferol derivatives
AssigneeBasilea Pharmaceutica AG
InventorHans Hilpert
Life of this patent
Estimating the term…
Abstract
A new process prepares retiferol derivatives of formula I: wherein A is —C ≡C— or —CH═CH—, and R1 and R2 are independently of each other lower alkyl or lower perfluoroalkyl, one version couples ketones of formula 1I with compounds of formula III A second version couples phosphinoxides of formula IV with aldehydes of formula V. Compounds of formula I are useful in the treatment or prevention of hyperproliferative skin diseases and for reversing the conditions associated with photodamage.
Claims5
A process for preparing a compound of the formula:
- wherein A is —C≡C— or —CH═CH— and
- R1 and R2 each independently are lower alkyl or lower perfluoroalkyl;
- which comprises coupling a compound of the formula:
- wherein X1 and X2 are hydroxy protecting (groups, with a compound of the formula:
- wherein A, R1, R2 are as above and Y is a hydroxy protecting group, to produce the compound of formula I.
2 more elements
A process for preparing a compound of the formula:
- wherein R1 and R2 are each independently lower alkyl or lower perfluoroalkyl;
- which comprises:
- a) coupling a compound of formula:
- wherein R3 is lower alkyl or mono-chlorinated lower alkyl, with a compound of formula:
- wherein R1, R2 are as above and Y is a Si(C1-4 -alkyl)3;
- and
- b) deprotecting the protected hydroxy groups to obtain a compound of formula Ia.
4 more elements
Dependencies are inferred from the claim text.